通过铜催化的叠氮-炔 1,3-偶极环加成反应进行肽-聚乙二醇化脂质偶联。
Peptide-Pegylated Lipid Conjugation Via Copper-Catalyzed Alkyne-Azide 1,3-Dipolar Cycloaddition.
机构信息
School of Chemistry and Molecular Biosciences, The University of Queensland, St. Lucia, QLD, Australia.
出版信息
Methods Mol Biol. 2021;2355:57-64. doi: 10.1007/978-1-0716-1617-8_6.
Targeted drug delivery is an important strategy in the treatment of many diseases. However, cancer cells are very difficult to target, making this a substantial obstacle in chemotherapy treatment. Bombesin fragment (BBN(6-14)) has been found to target gastrin-releasing peptide receptor (GRPR), which is overexpressed in many cancer cells. In this chapter, BBN peptide was used as a targeting moiety on the surface of polymeric-based nanoparticles to deliver its payload into prostate cancer PC-3 cell lines. Copper-catalyzed alkyne-azide 1,3-dipolar cycloaddition (CuAAC) click reaction was utilized to link the BBN peptide with an alkyne derivative of Pegylated lipid.
靶向药物输送是治疗许多疾病的重要策略。然而，癌细胞非常难以靶向，这使得化疗治疗成为一个巨大的障碍。蛙皮素片段（BBN（6-14））已被发现靶向胃泌素释放肽受体（GRPR），该受体在许多癌细胞中过度表达。在本章中，BBN 肽被用作聚合物基纳米粒子表面的靶向部分，将其有效载荷递送至前列腺癌 PC-3 细胞系中。铜催化的叠氮化物-炔烃 1,3-偶极环加成（CuAAC）点击反应被用于将 BBN 肽与 Pegylated 脂质的炔烃衍生物连接。
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